127308-82-1
127308-82-1 structure
- Name: Zamifenacin
- Chemical Name: (3R)-3-benzhydryloxy-1-[2-(1,3-benzodioxol-5-yl)ethyl]piperidine
- CAS Number: 127308-82-1
- Molecular Formula: C27H29NO3
- Molecular Weight: 415.52400
- Catalog: Signaling Pathways GPCR/G Protein mAChR
- Create Date: 2016-05-01 06:26:16
- Modify Date: 2024-01-09 17:42:06
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Zamifenacin (UK-76654) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome[1].
| Name | (3R)-3-benzhydryloxy-1-[2-(1,3-benzodioxol-5-yl)ethyl]piperidine |
|---|---|
| Synonyms |
Zamifenacin
UNII-Y88Q418Y7M |
| Description | Zamifenacin (UK-76654) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome[1]. |
|---|---|
| Related Catalog | |
| Target |
Muscarinic M3 receptor[1] |
| In Vivo | Zamifenacin exhibits moderate oral bioavailability (mouse 26%, rat 64%, dog 100%) and Cmax (mouse 92, rat 905, dog 416 ng/mL) following oral administration (mouse 13.2, rat 20 and, dog 5 mg/kg)[2]. Zamifenacin exhibits terminal elimination half-lives (mouse 2.1, rat 6.0 and, dog 1.1 h) due to high plasma clearance (68, 35, and 39 mL/min/kg respectively combined with large volumes of distribution (12.5, 19.0, and 3.5 L/kg respectively) following intravenous administration (mouse 5.3, rat 5.0 and, dog 1.0 mg/kg)[2]. Animal Model: Male CDl mice (mean weight 23 g)[2] Dosage: 5.3 mg/kg for i.v.; 13.2 mg/kg for oral (Pharmacokinetic Analysis) Administration: Intravenous administration and oral administration Result: Oral bioavailability (26%), Cmax (92 ng/mL), T1/2 (2.1 h). Animal Model: Male and female CD rats (mean weight 210 g)[2] Dosage: 5.0 mg/kg for i.v.; 20 mg/kg for oral (Pharmacokinetic Analysis) Administration: Intravenous administration and oral administration Result: Oral bioavailability (64%), Cmax (905 ng/mL), T1/2 (6.0 h). Animal Model: Male and two female beagle dogs (13-16 kg)[2] Dosage: 1.0 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis) Administration: Intravenous administration and oral administration Result: Oral bioavailability (100%), Cmax (416 ng/mL), T1/2 (1.1 h). |
| References |
| Density | 1.2g/cm3 |
|---|---|
| Boiling Point | 532.5ºC at 760mmHg |
| Molecular Formula | C27H29NO3 |
| Molecular Weight | 415.52400 |
| Flash Point | 145.6ºC |
| Exact Mass | 415.21500 |
| PSA | 30.93000 |
| LogP | 5.16630 |